Therapeutic compounds and uses thereof

Patent metadata

Field	Value
Publication number	US-11247989-B2
Application number	US-201816198581-A
Country	US
Kind code	B2
Filing date	Nov 21, 2018
Priority date	May 24, 2016
Publication date	Feb 15, 2022
Grant date	Feb 15, 2022

Abstract

The present invention relates to a compound formula (I):

and to salts thereof, wherein R 1 , R 2 X, and Y have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

First claim

We claim:

1. A compound of formula (Ia):

or a salt thereof, wherein:
R 1 is

R 2 is —C(O)—N(R e ) 2 , or —C(O)—R e ;
Y is selected from the group consisting of:

each R e is independently selected from hydrogen, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, and C 2-5 cycloalkyl, wherein each C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, and C 2-5 cycloalkyl is optionally substituted with one or more groups independently selected from oxo, halo, amino, hydroxyl, C 1-3 alkoxy, and C 1 -C 3 alkyl that is optionally substituted with one or more groups independently selected from halo.

2. The compound or salt of claim 1 wherein R 1 is

3. The compound or salt of claim 1 wherein Y is selected from the group consisting of:

4. The compound or salt of claim 1 wherein Y is selected from the group consisting of:

5. A compound or salt thereof selected from the group consisting of:

or a salt thereof.

6. A composition comprising a compound as described in claim 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable adjuvant, carrier, or vehicle.

7. A method for treating a CBP and/or EP300-mediated cancer in an animal by selectively inhibiting a bromodomain of the CBP and/or EP300 in the animal, comprising administering an effective amount of a compound or a pharmaceutically acceptable salt thereof, as described in claim 1 , to the animal, wherein the animal has a mutation in the CBP and/or EP300, and wherein the cancer is selected from lung cancer, breast cancer, pancreatic cancer, colorectal cancer,

Assignees

• Genentech Inc
• Constellation Pharmaceuticals Inc

Inventors

• Cyr Patrick
• Bronner Sarah
• Romero F Anthony
• Magnuson Steven
• Tsui Vickie Hsiao-Wei
• Murray Jeremy M
• Wai John
• Lai Kwong Wah
• Wang Fei
• Chen Kevin X

Classifications

• C07D519/00

  Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00 · CPC title

• C07D471/04 Primary

  Ortho-condensed systems · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P31/04

  Antibacterial agents · CPC title

• A61P13/12

  of the kidneys · CPC title